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Results for "

DYRK1A/B

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (26) Apoptosis (4) Bcl-2 Family (2) c-Myc (2) Caspase (2) CDK (7) DNA/RNA Synthesis (2) GSK-3 (2) PARP (2) Reference Standards (1) Tau Protein (1)
By Research Areas:	Cancer (18) Inflammation/Immunology (3) Metabolic Disease (4) Neurological Disease (8)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-X0009

Tambiciclib 1 Publications Verification GFH009; JSH-009; SLS009	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Metabolic Disease Inflammation/Immunology Cancer
Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over *DYRK1A*/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research .

HY-112296

T025 4 Publications Verification	CDK Apoptosis DYRK	Cancer
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with K_d values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC₅₀ values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .

HY-108476

INDY 2 Publications Verification	DYRK	Cancer
INDY is a potent and ATP-competitive *Dyrk1A* and *Dyrk1B* inhibitor with IC₅₀s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a K_i value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .

HY-111380

EHT 1610 2 Publications Verification	DYRK	Neurological Disease
EHT 1610 is a potent inhibitor of *DYRK, with IC₅₀s* of 0.36 nM (DYRK1A), 0.59 nM (DYRK1B), respectively. EHT 1610 exhibits antileukemia effect, regulates cell cycle and induces cell apoptosis ^- .

HY-15951

ML167 CID44968231; NCGC00188654	CDK DYRK	Cancer
ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC₅₀ of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B .

HY-155723

Leucettinib-92	CDK DYRK	Others
Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC₅₀s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3) .

HY-12838

RO5454948 1 Publications Verification Mirk-IN-1; DYRK1B/A-IN-1	DYRK	Cancer
RO5454948 (Compound 9) is the inhibitor for *Dyrk1B* and *Dyrk1A* with IC₅₀ of 68 nM and 22 nM. RO5454948 exhibits cytotoxicity in cancer cell SW620 with EC₅₀ of 1.9 μM .

HY-146221

Dyrk1A-IN-5 1 Publications Verification	DYRK	Neurological Disease
Dyrk1A-IN-5 (Compound 5j) is a potent and selective *DYRK1A* inhibitor, with an IC₅₀ of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC₅₀ = 600 nM) and CLK1 (IC₅₀ = 500 nM), but shows almost no inhibition of DYRK2 (IC₅₀ > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research .

HY-111379

EHT 5372	DYRK CDK GSK-3	Neurological Disease Metabolic Disease Cancer
EHT 5372 is a highly potent and selective inhibitor of *DYRK's* family kinases with IC₅₀s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for *DYRK1A, DYRK1B, DYRK2, DYRK*3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .

HY-147060

Dyrk1A-IN-3	DYRK	Neurological Disease
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC₅₀=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .

HY-128758A

DYRKs-IN-1 hydrochloride	DYRK	Cancer
DYRKs-IN-1 hydrochloride is a potent *DYRKs* (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity .

HY-144614

JH-XVII-10	DYRK Apoptosis	Neurological Disease Cancer
JH-XVII-10 is a potent, selective and orally active *DYRK1A* and *DYRK1B* inhibitor with IC₅₀s of 3 nM and 5 nM for *DYRK1A* and *DYRK1B*, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .

HY-77324S

4-(Trifluoromethyl)aniline-d4 4-Aminobenzotrifluoride-d₄	DYRK	Cancer
4-(Trifluoromethyl)aniline-d₄ (4-Aminobenzotrifluoride-d₄) is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC₅₀s of 54.84 nM and 186.40 nM, respectively .

HY-108475

ProINDY	DYRK	Cancer
ProINDY, a prodrug of INDY (HY-108476), is a *DYRK1A* and *DYRK1B* inhibitor. ProINDY effectively recovers Xenopus embryos from head malformation induced by Dyrk1A overexpression .

HY-146337

Dyrk1A/B-IN-1	DYRK	Cancer
Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable *DYRK1A* and *DYRK1B* inhibitor with K_is of 67.8 nM and 237.9 nM, and IC₅₀s of 1.1 μM and 0.8 μM, respectively. Dyrk1A/B-IN-1 is not toxic to human cells. Dyrk1A/B-IN-1 can be used for researching DYRK1A and DYRK1B cellular functions and their role in pathologies .

HY-144617

JH-XIV-68-3	DYRK	Cancer
JH-XIV-68-3 is a selective macrocyclic inhibitor of *DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A* and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines .

HY-128759

DYRKs-IN-2	DYRK	Cancer
DYRKs-IN-2 (Example 132) is a potent *DYRKs* inhibitor with IC₅₀s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity .

HY-128758

DYRKs-IN-1	DYRK	Cancer
DYRKs-IN-1 is a potent *DYRKs* (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity .

HY-X0009A

Tambiciclib dimaleate 1 Publications Verification GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate	CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis	Cancer
Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over *DYRK1A*/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research .

HY-159496

Dyrk1A-IN-10	DYRK	Metabolic Disease
Dyrk1A-IN-10 (compound B4) is a *DYRK1A* inhibitor with antidiabetic activity. Dyrk1A-IN-10 can promote pancreatic β-cell proliferation, increase insulin secretion, and lower blood sugar .

HY-144695

Dyrk1A/α-synuclein-IN-1	DYRK	Neurological Disease
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual *Dyrk1A* and α-synuclein aggregation inhibitor with IC₅₀ values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .

HY-144696

Dyrk1A/α-synuclein-IN-2	DYRK	Neurological Disease
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual *Dyrk1A* and α-synuclein aggregation inhibitor with an IC₅₀ of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .

HY-183955

GNF7156	DYRK GSK-3	Metabolic Disease Inflammation/Immunology
GNF7156 is a *DYRK1A/GSK3B* inhibitor, IC₅₀ values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes .

HY-181085

RD0448	DYRK	Neurological Disease Inflammation/Immunology Cancer
RD0448 is a potent inhibitor of *DYRK1A, DYRK1B, and DYRK2. RD0448 selectively targets the non-native (folded intermediate) state of DYRK1A* and DYRK1B. The binding site of RD0448 is hidden in the native state of DYRK1A and DYRK1B, and as a stabilizing binder, it binds tightly to both DYRK1A and DYRK1B, forming a stable complex with slow dissociation kinetics. In contrast, RD0448 targets the native state of DYRK2 without selectivity between its native and non-native states, acting as a weak binder with weaker binding affinity to DYRK2 and forming a rapidly dissociating complex .

HY-108476R

INDY (Standard)	Reference Standards DYRK	Cancer
INDY (Standard) is the analytical standard of INDY (HY-108476). This product is intended for research and analytical applications. INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC₅₀s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a K_i value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells .

HY-402805

DYRK2-IN-2	DYRK CDK Tau Protein	Cancer
DYRK2-IN-2 (Compound C17) is a selective inhibitor of *DYRK2, with its IC₅₀* value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on *DYRK1A* (IC₅₀ = 1842 nM), *DYRK1B* (IC₅₀ = 1335 nM), *DYRK4* (IC₅₀ = 1931 nM), *DYRK3* (IC₅₀ = 112 nM), and CLKs (IC₅₀ = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research .

4-(Trifluoromethyl)aniline-d4
4-(Trifluoromethyl)aniline-d₄ (4-Aminobenzotrifluoride-d₄) is deuterium labeled 4-(Trifluoromethyl)aniline. 4-(Trifluoromethyl)aniline is a DYRK1A and DYRK1B kinase inhibitor with IC₅₀s of 54.84 nM and 186.40 nM, respectively .

Cat. No.	Product Name		Classification

HY-181085

RD0448		Alkynes
RD0448 is a potent inhibitor of *DYRK1A, DYRK1B, and DYRK2. RD0448 selectively targets the non-native (folded intermediate) state of DYRK1A* and DYRK1B. The binding site of RD0448 is hidden in the native state of DYRK1A and DYRK1B, and as a stabilizing binder, it binds tightly to both DYRK1A and DYRK1B, forming a stable complex with slow dissociation kinetics. In contrast, RD0448 targets the native state of DYRK2 without selectivity between its native and non-native states, acting as a weak binder with weaker binding affinity to DYRK2 and forming a rapidly dissociating complex .

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